ChemicalBook > CAS DataBase List > RGB-286638

RGB-286638

Product Name
RGB-286638
CAS No.
784210-87-3
Chemical Name
RGB-286638
Synonyms
CS-1713;RGB-286638;RGB-286638 Dihydrochloride;N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea hydrochloride
CBNumber
CB62667740
Molecular Formula
C29H37Cl2N7O4
Formula Weight
618.55458
MOL File
784210-87-3.mol
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RGB-286638 Property

storage temp. 
Store at -20°C
solubility 
DMSO: ≥ 150 mg/mL (242.50 mM)
form 
Powder
color 
Light yellow to yellow
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

American Custom Chemicals Corporation
Product number
API0017268
Product name
RGB-286638
Purity
95.00%
Packaging
5MG
Price
$497.62
Updated
2021/12/16
ChemScene
Product number
CS-3453
Product name
RGB-286638
Purity
98.72%
Packaging
50mg
Price
$1320
Updated
2021/12/16
ChemScene
Product number
CS-3453
Product name
RGB-286638
Purity
98.72%
Packaging
100mg
Price
$2400
Updated
2021/12/16
Crysdot
Product number
CD31000796
Product name
RGB-286638
Purity
98+%
Packaging
5mg
Price
$116
Updated
2021/12/16
Crysdot
Product number
CD31000796
Product name
RGB-286638
Purity
98+%
Packaging
10mg
Price
$193
Updated
2021/12/16
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RGB-286638 Chemical Properties,Usage,Production

Uses

RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.

in vivo

Dose-finding studies with RGB-286638 identify 40 mg/kg/day IV treatment as the maximum tolerated dose in SCID mice. Five days IV treatment with RGB-286638 significantly suppresses MM tumor growth, with maximum TGI (%) noted at day 14 following end of treatment at 85.06% and 86.34% in the 30 mg/kg and 40 mg/kg treated cohorts respectively. The log10 cell kill (LCK Td: 4.5 days) is 1.6 for both treated groups. RGB-286638 treatment is also associated with improved survival, evidenced by first death at day 24 in controls versus day 43 in both treated groups. No toxic deaths occurred during this study: maximum percentage of body weight (BW) loss is observed on day 5 (8.4%) at 30 mg/kg dosage schedule, and on day 15 (9.9%) after 40 mg/kg dosing, with weight recovery in the following two weeks[1].

IC 50

T1-CDK9: 1 nM (IC50); cyclin B1-CDK1: 2 nM (IC50); cyclin E-CDK2: 3 nM (IC50); cyclin D1-CDK4: 4 nM (IC50); cyclin E-CDK3: 5 nM (IC50); p35-CDK5: 5 nM (IC50); cyclin H-CDK7: 44 nM (IC50); cyclin D3-CDK6: 55 nM (IC50); GSK-3β: 3 nM (IC50); JAK2: 50 nM (IC50); MEK1: 54 nM (IC50); Fms: 1 nM (IC50); TAK1: 5 nM (IC50); JNK1a1: 17 nM (IC50); JNK1a2: 40 nM (IC50); C-src: 25 nM (IC50); AMPK: 41 nM (IC50)

References

[1] Cirstea D, et al. Small-molecule multi-targeted kinase inhibitor RGB-286638 triggers P53-dependent and -independent anti-multiple myeloma activity through inhibition of transcriptional CDKs. Leukemia. 2013 Dec;27(12):2366-75. DOI:10.1038/leu.2013.194

RGB-286638 Preparation Products And Raw materials

Raw materials

Preparation Products

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RGB-286638 Suppliers

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784210-87-3, RGB-286638Related Search:


  • N-[1,4-Dihydro-3-[4-[[4-(2-methoxyethyl)-1-piperazinyl]methyl]phenyl]-4-oxoindeno[1,2-c]pyrazol-5-yl]-N'-4-morpholinylurea hydrochloride
  • RGB-286638
  • CS-1713
  • RGB-286638 Dihydrochloride
  • 784210-87-3
  • C29H35N7O42HCl